Development of a clickable bimodal fluorescent/PET probe for in vivo imaging.
Development of a clickable bimodal fluorescent/PET probe for in vivo imaging.
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DOI：
10.1186/s13550-015-0120-4
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发表时间：
2015-12
期刊：
影响因子：
3.2
通讯作者：
Weber WA
中科院分区：
文献类型：
--
作者：
Paulus A;Desai P;Carney B;Carlucci G;Reiner T;Brand C;Weber WA
荧光成像剂在临床前和临床研究中变得越来越重要。然而，它们的组织穿透性很差，这使得光学荧光成像与全身成像技术不兼容。因此，新型双峰PET活性和荧光示踪剂的设计可以将光学成像的益处与放射性标记的成像探针联合收割机结合。在此，我们报告了可点击的18F标记的荧光染料的合成和评价。叠氮化物修饰的BODIPY-Fl染料可以使用BODIPY染料的硼-氟化物核心的18F/19 F交换反应成功地用18F放射性标记，以产生可点击的双峰PET/荧光成像工具。使用蛙皮素类似物进行体外和体内成像（PET/荧光），以研究双模态成像探头的适用性。我们使用放射性标记的小分子，18F-BODIPY-叠氮化物标记位点特异性不同的靶向肽，基于标准的模块化标记协议。双峰蛙皮素类似物的合成后，我们确定肽示踪剂在体外和体内的性能，探索光学以及PET成像能力。这种多功能的方法有可能对18F放射性示踪剂的合成产生变革性的影响，为在细胞（光学）和全身（PET）水平上快速筛选新型标记的肽示踪剂打开了大门。本文的在线版本（doi：10.1186/s13550-015-0120-4）包含补充材料，可供授权用户使用。
Fluorescent imaging agents are becoming evermore important in preclinical and clinical research. They do, however, suffer from poor tissue penetration, which makes optical fluorescence imaging incompatible with whole-body imaging techniques. The design of novel bimodal PET active and fluorescent tracers could therefore combine the benefits of optical imaging with radioactively labeled imaging probes. Herein, we report the synthesis and evaluation of a clickable 18F-labeled fluorescent dye. An azide-modified BODIPY-Fl dye could be successfully radio-labeled with 18F using an 18F/19F exchange reaction of the boron-fluoride core of the BODIPY dye to yield a clickable bimodal PET/fluorescent imaging tool. In vitro as well as in vivo imaging (PET/fluorescence) using a bombesin analog was conducted to study the applicability of the dual-modality imaging probe. We use the radio-labeled small molecule, 18F-BODIPY-azide to label site-specifically different targeted peptides, based on a standard modular labeling protocol. Following the synthesis of a bimodal bombesin analog, we determine the peptide tracer’s performance in vitro and in vivo, exploring both the optical as well as PET imaging capabilities. This versatile methodology has the potential to have a transformational impact on 18F radiotracer synthesis, opening the door for rapid screening of novel-labeled peptide tracers, both on the cellular (optical) as well as whole-body (PET) level. The online version of this article (doi:10.1186/s13550-015-0120-4) contains supplementary material, which is available to authorized users.